DOCSLIB.ORG

Thin-Layer Chromatographic Analysis of Steroids: a Review

Total Page：16

File Type：pdf, Size：1020Kb

Download full-text PDF Read full-text
Thin-Layer Chromatographic Analysis of Steroids: a Review Bhawani et al Tropical Journal of Pharmaceutical Research June 2010; 9 (3): 301-313 © Pharmacotherapy Group, Faculty of Pharmacy, University of Benin, Benin City, 300001 Nigeria. All rights reserved . Available online at http://www.tjpr.org Review Article Thin-Layer Chromatographic Analysis of Steroids: A Review SA Bhawani* 1, O Sulaiman 1, R Hashim 1 and MN Mohamad Ibrahim 2 1Division of Bio-Resource, Paper and Coatings Technology, School of Industrial Technology, 2School of Chemical Sciences, Universiti Sains Malaysia, 11800, Pulau Pinang, Malaysia Abstract Thin layer chromatography has been used for the analysis of natural and synthetic steroids in various environmental materials. This review focuses mainly on steroid analysis in environmental materials such as pharmaceuticals, plant products and other biological specimens. The most widely investigated biological specimens are urine and blood plasma or serum. Various chromatographic systems useful for the identification; separation and quantification of surfactants are also reported in this review. Keywords: Steroids; Thin layer chromatography; Environmental materials; Biological specimens Received: 15 November 2009 Revised accepted: 18 March 2010 *Corresponding author: E-mail: [email protected] Trop J Pharm Res, June 2010; 9 (3): 301 Bhawani et al INTRODUCTION androgens. Steroids, such as nandrolone, dromostanolone, stanozolol, are often used Steroids are terpenoid lipids characterized by illegally to increase the performance of the sterane or steroid nucleus: a carbon competitive athletes of almost all age groups. skeleton with four fused rings, generally They are banned in most sports competitions arranged in a 6-6-6-5 fashion. Steroids vary such as the Olympic Games. by the functional groups attached to these rings and the oxidation state of the rings. The Classification of Steroids specificity of their different biological actions is due to the various groups attached to a Steroids have been classified into a number common nucleus. When alcohol groups (OH) of groups by Scott [1] based on their are attached, steroids should properly be functions as follows: (i) sterols and steroid called sterols (e.g., cortisol), whereas ketone alcohols, usually with double bonds; (ii) sex groups (C=O) make them sterones (e.g., hormones - steroids produced mainly in the aldosterone). testis (androgens) or ovary (estrogens); (iii) adrenocortical hormones - steroids produced Steroids comprise a large group of in the cortex of the adrenal gland; (iv) bile substances that mediate a very varied set of acids - steroids usually bonded to taurine or biological responses. The most widespread in glycine and functioning as emulsion- the body is cholesterol, an essential stabilizing agents in the intestine; (v) component of cell membranes and the sapogenins - plant products with a steroid starting point for the synthesis of other bonded to carbohydrates; (vi) cardiac steroids - sex hormones, adrenal cortical glycosides - plant products similar to hormones, and the bile salts. Steroids (e..g., sapogenins and used as heart stimulants; glucocorticoids, mineralocorticoids, and (vii) vitamin D androgens,estrogens and progestagens) have major responsibilities as hormones, ANALYSIS OF STEROIDS controlling metabolism, salt balance, and the development and function of the sexual Many procedures used for the quality control organs as well as other biological differences and quality assurance of steroids are based between the sexes. Steroids in the form of on classical methods of analysis. However, bile salts (e.g., salts of cholic and deoxycholic the need for improved precision and accuracy acid and their glycine and taurine conjugates) has led to the increased use of instrumental assist in digestive processes, while another analysis. Thus, the development of fast and steroid is a vitamin (calcitriol) that takes part reliable analytical methods for quality control, in calcium control. Steroids (naturally including the identification of synthesis by- occurring or synthetic) such as products and purity tests, are both important methylprednisolone, hydrocortisone, gluco- and challenging. Thin-layer chromatography cortisteroids, corticosteroids, squalamine, (TLC) continues to be an important method oestrogens, androgens, are also used for the for qualitative analysis of steroids because of treatment of various diseases such as allergic its inherent advantages - many samples can reactions, arthritis, some malignancies, and be analyzed simultaneously and quickly, and diseases resulting from hormone deficiencies multiple separation techniques and detection or abnormal production. In addition, synthetic procedures can be applied. This review steroids (e.g., mifepristone) that mimic the presents the contribution of thin-layer action of progesterone are widely used as chromatography in the analysis of steroids oral contraceptive agents. Other synthetic from 1990-2009. It addresses most aspects steroids (e.g., oxandrolone) are designed to of thin-layer chromatography, including mimic the stimulation of protein synthesis and detection, separation and quantification of muscle-building action of naturally occurring steroids. Trop J Pharm Res, June 2010; 9 (3): 302 Bhawani et al Thin-layer chromatography of steroids TLC continues to be an important method for the determination of steroids because of its Szepesi and Gazdag wrote a book chapter advantages. Many samples can be analyzed on the TLC of steroids, and it included simultaneously and quickly at relatively low information on sample preparation as well as cost; also, multiple separation techniques and stationary-phase and mobile-phase systems detection procedures can be applied and the useful for the separation of steroidal detection limits are often in the low nanogram pharmaceuticals [2]. The authors also range, and quantitative densitometric provided detailed methods of detection and methods are accurate. Modern approaches in quantification of steroids, and later on, thin-layer chromatography enable analysts to updated their review to include coverage separate and determine steroids in complex through 1994 [3]. Dreassi et al [4] have also mixtures, including various environmental reviewed the application of TLC to steroids in samples. Steroids and their metabolites are pharmaceutical analysis while Jain has analyzed by thin-layer chromatography in a provided some information on the analysis of variety of samples such as biological steroid hormones in his review on TLC in samples, plants and pharmaceutical clinical chemistry [5]. formulations. Table 1(a)-(e) shows several thin-layer chromatographic systems designed for the analysis of steroids [6-29]. Table 1(a): Thin-layer chromatographic analysis of steroids Analyte Stationar Mobile phase Remarks Ref y phase Cholestrol, RP- Acetronitrile/methanol, Investigation of the retention behavior 6 allylestrenol, HPTLC acetronitrile/water and of 12 sreroids.Mixture of 10g copper pregnanediol, plates methanol/water in different binary sufate and 5 mL o-phosphoric acid etc. mixtures (86%) dissolved in 95 mL methanol. Androgens Silica Cyclohaxane/ethylacetate/ethanol HPTLC separation of anabolic and gestagens (24:16:1) and Androgens. chloroform/benzene/ethanol(36:4:1 Detected by fluorescence after ) in one direction immersion in a 5% sulfuric acid-ethanol ;chloroform/acetone (9:1) and solution for 30 sec and viewed under hexane/dichloromethane/ UV366nm. acetronitrile (4:3:2) in second direction for androgens and gestagens respectively Steroids Silica Chloroform/ethanol/water Detection under 8 (188:12:1) UV.Quantification by radioimmunoassay. Progesterone, Silica Methanol/ethylacetate/chloroform/ Programmed multiple development of 9 testosterone, methylenechloride (first inverse analysis of steroids. testosterone gradient program) and Detected under UV 254.Densitometry hydrogen methanol/chloroform (second was used for the quantification. sulfate sodium inverse gradient program) salt, etc. Oxo-steroids Silica gel Chloroform/methanol (97:3) Measurement of 17-oxo steroids in biol. 10 F254 Fluids with TLC and fluorometric scanning detection. Dansylhydrazine was used as a prelabeling reagent. Linearity of fluorescence detection was obtained at 30-1000 ng. Trop J Pharm Res, June 2010; 9 (3): 303 Bhawani et al Table 1(b): Thin-layer chromatographic analysis of steroids ( contd. ) Analyte Stationary Mobile phase Ref phase Hydrocortisone, Benzene/ Use of colour 11 prednisolone, ethylacetate (1:1) photodocumentation of UV- mesylate, etc. irradiated thin-layer chromatograms for the analysis of steroids.Detected by spraying with a 10% ethanolic solution of sulfuric acid followed by heating at 100 oC for 2 to 4 min Anabolic steroids Silica Chloroform/aceto Analysis of anabolic steroids by 12 ne (9:1) in one high-performance thin-layer direction and chromatography.Detected by cyclohexane/ethy spraying with 10% sulfuric acid in lacetate/methano methanol and heating for 10 min at l (117:78:11) in 95 oC in day light and under UV the opposite 366nm.Further confirmation was direction done by GC-MS Cortisone, NH 2 F 245s Chloroform/ethan Analysis and separation of steroids 13 hydrocortisone, ol/formic acid on NH 2 layers. estradiol, (50:10:10), Estradiol benzoate, Chloroform/meth estriol,estrone, anol (95:5), methyltestosterone, Chloroform/1- testosterone, propanol/formica testosterone cid (50:10:5) propionate, prednisolone, pegnandiol and triol, progeterone and Reichstein’s S Cortisole, cortisone, NH 2 F 245s Chloroform/ethan Separation
Load more

Recommended publications
  • Aldrich FT-IR Collection Edition I Library
    Aldrich FT-IR Collection Edition I Library Library Listing – 10,505 spectra This library is the original FT-IR spectral collection from Aldrich. It includes a wide variety of pure chemical compounds found in the Aldrich Handbook of Fine Chemicals. The Aldrich Collection of FT-IR Spectra Edition I library contains spectra of 10,505 pure compounds and is a subset of the Aldrich Collection of FT-IR Spectra Edition II library. All spectra were acquired by Sigma-Aldrich Co. and were processed by Thermo Fisher Scientific. Eight smaller Aldrich Material Specific Sub-Libraries are also available. Aldrich FT-IR Collection Edition I Index Compound Name Index Compound Name 3515 ((1R)-(ENDO,ANTI))-(+)-3- 928 (+)-LIMONENE OXIDE, 97%, BROMOCAMPHOR-8- SULFONIC MIXTURE OF CIS AND TRANS ACID, AMMONIUM SALT 209 (+)-LONGIFOLENE, 98+% 1708 ((1R)-ENDO)-(+)-3- 2283 (+)-MURAMIC ACID HYDRATE, BROMOCAMPHOR, 98% 98% 3516 ((1S)-(ENDO,ANTI))-(-)-3- 2966 (+)-N,N'- BROMOCAMPHOR-8- SULFONIC DIALLYLTARTARDIAMIDE, 99+% ACID, AMMONIUM SALT 2976 (+)-N-ACETYLMURAMIC ACID, 644 ((1S)-ENDO)-(-)-BORNEOL, 99% 97% 9587 (+)-11ALPHA-HYDROXY-17ALPHA- 965 (+)-NOE-LACTOL DIMER, 99+% METHYLTESTOSTERONE 5127 (+)-P-BROMOTETRAMISOLE 9590 (+)-11ALPHA- OXALATE, 99% HYDROXYPROGESTERONE, 95% 661 (+)-P-MENTH-1-EN-9-OL, 97%, 9588 (+)-17-METHYLTESTOSTERONE, MIXTURE OF ISOMERS 99% 730 (+)-PERSEITOL 8681 (+)-2'-DEOXYURIDINE, 99+% 7913 (+)-PILOCARPINE 7591 (+)-2,3-O-ISOPROPYLIDENE-2,3- HYDROCHLORIDE, 99% DIHYDROXY- 1,4- 5844 (+)-RUTIN HYDRATE, 95% BIS(DIPHENYLPHOSPHINO)BUT 9571 (+)-STIGMASTANOL
    [Show full text]
  • Ocps) Used in the NM Family Planning Program (FPP
    The following slides are intended to familiarize nurses and clinicians with oral contraceptive pills (OCPs) used in the NM Family Planning Program (FPP). The FPP does not intend for this information to supersede the Family Planning Protocol particularly on the requirement for Public Health Nurses in the Public Health Offices to consult a clinician as stated in the Protocol when in doubt or if it is necessary to switch the client’s OCP type. 1 2 Combined oral contraceptives (COCs) contain two hormones; estrogen and progestin. In general, any combined OCP is good for most women who are eligible to take estrogen according to the CDC U.S. Medical Eligibility Criteria (MEC). Once again, refer to the US MEC chart to find out if OCP is a suitable choice for clients with specific health conditions. To learn a little bit about what each hormone does, the FPP is providing the following summary: Estrogen: provides endometrial stability = menstrual cycle control. A higher estrogen dose increases the venous thromboembolism (VTE) or clot risk but OCP clot risk is still less harmful than the clot risk related to pregnancy and giving birth. Progestin: provides most of the contraceptive effect by ‐Preventing luteinizing hormone (LH) surge /ovulation ‐Thickening the cervical mucus to prevent sperm entry. Two major OCP formations are available. Monophasic: There is only one dose of estrogen and progestin in each active pill in the packet; and Multiphasic: There are varying doses of hormones, particularly progestin in the active pills. 3 Section 3 of the FPP Protocol contains the OCP Substitute Table, which groups OCPs into 6 classes according to the estrogen dosage, the type of progestin and the formulations.
    [Show full text]
  • Record of Reasons for 16-18 November 1999 Meeting
    1 NATIONAL DRUGS AND POISONS SCHEDULE COMMITTEE MEETING 25 – 16-18 November 1999 RECORD OF REASONS FOR AMENDMENT TO THE STANDARD FOR THE UNIFORM SCHEDULING OF DRUGS AND POISONS AGRICULTURAL, VETERINARY AND DOMESTIC CHEMICALS Buprofezin – Schedule required Amendment and Reasons The decision below was based on buprofezin’s toxicological profile, in particular its acute oral toxicity. A cut-off to exempt at a concentration of 40% was agreed because of the reduced oral toxicity at this concentration and the ability of safety directions and warning statements applied through the registration system for agricultural and veterinary chemicals to adequately address the slight eye irritation which was attributed to the product formulation. Schedule 5 – New entry BUPROFEZIN except in preparations containing 40 per cent or less of buprofezin. Copper hydroxide - progression of foreshadowed decision to include copper hydroxide in Schedule 6 with cut-off to Schedule 5 at 50 per cent and to exempt at 12.5 per cent. Amendment and Reasons The amendment below was based on the acute oral toxicity of copper hydroxide, its severe eye irritancy / corrosivity, and the possibility of products containing copper hydroxide being accessible in domestic situations and therefore presenting a risk of accidental ingestion. Schedule 6 – New entry COPPER HYDROXIDE except: (a) when included in Schedule 5; or (b) in preparations containing 12.5 per cent or less of copper hydroxide. Schedule 5 – New entry COPPER HYDROXIDE in preparations containing 50 per cent or less of copper hydroxide except in preparations containing 12.5 per cent or less of copper hydroxide. Cyhexatin - Review of Appendix F warning statements and Appendix J rider.
    [Show full text]
  • (12) Patent Application Publication (10) Pub. No.: US 2006/0110428A1 De Juan Et Al
    US 200601 10428A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2006/0110428A1 de Juan et al. (43) Pub. Date: May 25, 2006 (54) METHODS AND DEVICES FOR THE Publication Classification TREATMENT OF OCULAR CONDITIONS (51) Int. Cl. (76) Inventors: Eugene de Juan, LaCanada, CA (US); A6F 2/00 (2006.01) Signe E. Varner, Los Angeles, CA (52) U.S. Cl. .............................................................. 424/427 (US); Laurie R. Lawin, New Brighton, MN (US) (57) ABSTRACT Correspondence Address: Featured is a method for instilling one or more bioactive SCOTT PRIBNOW agents into ocular tissue within an eye of a patient for the Kagan Binder, PLLC treatment of an ocular condition, the method comprising Suite 200 concurrently using at least two of the following bioactive 221 Main Street North agent delivery methods (A)-(C): Stillwater, MN 55082 (US) (A) implanting a Sustained release delivery device com (21) Appl. No.: 11/175,850 prising one or more bioactive agents in a posterior region of the eye so that it delivers the one or more (22) Filed: Jul. 5, 2005 bioactive agents into the vitreous humor of the eye; (B) instilling (e.g., injecting or implanting) one or more Related U.S. Application Data bioactive agents Subretinally; and (60) Provisional application No. 60/585,236, filed on Jul. (C) instilling (e.g., injecting or delivering by ocular ion 2, 2004. Provisional application No. 60/669,701, filed tophoresis) one or more bioactive agents into the Vit on Apr. 8, 2005. reous humor of the eye. Patent Application Publication May 25, 2006 Sheet 1 of 22 US 2006/0110428A1 R 2 2 C.6 Fig.
    [Show full text]
  • Hormonal Treatment Strategies Tailored to Non-Binary Transgender Individuals
    Journal of Clinical Medicine Review Hormonal Treatment Strategies Tailored to Non-Binary Transgender Individuals Carlotta Cocchetti 1, Jiska Ristori 1, Alessia Romani 1, Mario Maggi 2 and Alessandra Daphne Fisher 1,* 1 Andrology, Women’s Endocrinology and Gender Incongruence Unit, Florence University Hospital, 50139 Florence, Italy; [email protected] (C.C); jiska.ristori@unifi.it (J.R.); [email protected] (A.R.) 2 Department of Experimental, Clinical and Biomedical Sciences, Careggi University Hospital, 50139 Florence, Italy; [email protected]fi.it * Correspondence: fi[email protected] Received: 16 April 2020; Accepted: 18 May 2020; Published: 26 May 2020 Abstract: Introduction: To date no standardized hormonal treatment protocols for non-binary transgender individuals have been described in the literature and there is a lack of data regarding their efficacy and safety. Objectives: To suggest possible treatment strategies for non-binary transgender individuals with non-standardized requests and to emphasize the importance of a personalized clinical approach. Methods: A narrative review of pertinent literature on gender-affirming hormonal treatment in transgender persons was performed using PubMed. Results: New hormonal treatment regimens outside those reported in current guidelines should be considered for non-binary transgender individuals, in order to improve psychological well-being and quality of life. In the present review we suggested the use of hormonal and non-hormonal compounds, which—based on their mechanism of action—could be used in these cases depending on clients’ requests. Conclusion: Requests for an individualized hormonal treatment in non-binary transgender individuals represent a future challenge for professionals managing transgender health care. For each case, clinicians should balance the benefits and risks of a personalized non-standardized treatment, actively involving the person in decisions regarding hormonal treatment.
    [Show full text]
  • Comparing the Effects of Combined Oral Contraceptives Containing Progestins with Low Androgenic and Antiandrogenic Activities on the Hypothalamic-Pituitary-Gonadal Axis In
    JMIR RESEARCH PROTOCOLS Amiri et al Review Comparing the Effects of Combined Oral Contraceptives Containing Progestins With Low Androgenic and Antiandrogenic Activities on the Hypothalamic-Pituitary-Gonadal Axis in Patients With Polycystic Ovary Syndrome: Systematic Review and Meta-Analysis Mina Amiri1,2, PhD, Postdoc; Fahimeh Ramezani Tehrani2, MD; Fatemeh Nahidi3, PhD; Ali Kabir4, MD, MPH, PhD; Fereidoun Azizi5, MD 1Students Research Committee, School of Nursing and Midwifery, Department of Midwifery and Reproductive Health, Shahid Beheshti University of Medical Sciences, Tehran, Islamic Republic Of Iran 2Reproductive Endocrinology Research Center, Research Institute for Endocrine Sciences, Shahid Beheshti University of Medical Sciences, Tehran, Islamic Republic Of Iran 3School of Nursing and Midwifery, Department of Midwifery and Reproductive Health, Shahid Beheshti University of Medical Sciences, Tehran, Islamic Republic Of Iran 4Minimally Invasive Surgery Research Center, Iran University of Medical Sciences, Tehran, Islamic Republic Of Iran 5Endocrine Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Islamic Republic Of Iran Corresponding Author: Fahimeh Ramezani Tehrani, MD Reproductive Endocrinology Research Center Research Institute for Endocrine Sciences Shahid Beheshti University of Medical Sciences 24 Parvaneh Yaman Street, Velenjak, PO Box 19395-4763 Tehran, 1985717413 Islamic Republic Of Iran Phone: 98 21 22432500 Email: [email protected] Abstract Background: Different products of combined oral contraceptives (COCs) can improve clinical and biochemical findings in patients with polycystic ovary syndrome (PCOS) through suppression of the hypothalamic-pituitary-gonadal (HPG) axis. Objective: This systematic review and meta-analysis aimed to compare the effects of COCs containing progestins with low androgenic and antiandrogenic activities on the HPG axis in patients with PCOS.
    [Show full text]
  • Endocrine Disrupting Compounds and Prostate Cell Proliferation
    Review Article Clinics in Oncology Published: 18 Oct, 2016 Endocrine Disrupting Compounds and Prostate Cell Proliferation Joubert Banjop Kharlyngdoh and Per-Erik Olsson* Department of Biology, Örebro University, Sweden Abstract Epidemiological, in vitro and animal studies have indicated that Endocrine Disrupting Compounds (EDCs) influence the normal growth and development of the prostate as well as development and progression of prostate cancer. This has been linked to an increased presence of environmental chemicals that interfere with hormonal signaling. Many of these effects appear to be associated with interferences with steroid hormone receptor signaling or by affecting steroidogenesis. Currently, there is abundant evidence from epidemiological studies linking pesticides and EDCs with elevated prostate cancer risk. Bisphenol-A, a known EDC, has been shown to promote induction of Prostate Specific Antigen (PSA), which is a biomarker for prostate cancer, in the LNCaP human prostate carcinoma cells, and to increase prostate carcinogenesis in animal models. Our research has focused on AR signaling and identification of novel androgenic and anti-androgenic EDCs. Using prostate cancer cell lines we have shown that the AR agonist, TBECH, and antagonist ATE, which is also a partial ART877A agonist, induce PSA expression. With the increasing presence of these EDCs in indoor and outdoor air, follows an increased risk of disturbed prostate development, regulation and function. Hence, identification of the contribution of EDCs to prostate cancer
    [Show full text]
  • 2013 House Judiciary Hb 1070
    2013 HOUSE JUDICIARY HB 1070 2013 HOUSE STANDING COMMITTEE MINUTES House Judiciary Committee Prairie Room, State Capitol HB 1070 January 14, 2013 Job #17167 D Conference Committee � · Committee Clerk Signature A-. .;' /) .1� ' I A.J4-��'N'f?4<'71<P2/ I Explanation or reason for introduction of bill/resolution: Relating to the scheduling of controlled substances. Minutes: Chairman Koppelman: Opened the hearing on HB 1070. Mark Hardy, Assistant Executive Director of the NO State Board of Pharmacy: (See testimony #1and 2) He went over these handouts. Rep. Klemin: I don't see an emergency clause in the bill and there is none in the amendment. Did I miss it? Mark Hardy: I want to put an emergency clause on the bill. Rep. Klemin: I think you have to have another section at the end of the bill saying this is an emergency. Rep. Kretschmar: How often do these new drugs come out and should be on it? Mark Hardy: As far as the schedule 1 substances; it is a revolving door and we are always trying to stay in front of what the chemists and what the drug makers are doing. As far as schedule 2 through 5; it is a continuous thing through the DEA. When it becomes a federally controlled substance it takes precedence. Rep. Larson: You have not been aware of the bill I was sponsoring regarding synthetic drugs yet? Mark Hardy: No. The Attorney General briefed me on the Bill #1133. Rep. Larson: The reason for my bill is not get into all of the pharmaceutical names of the chemicals, but anybody that possess or manufacturers a analog in order to try and copy these drugs would be guilty of those offences without having to know the specific chemical compound that might be morphed by unscrupulous people trying to see these products.
    [Show full text]
  • Effects of Zilpaterol and Melengestrol Acetate On
    EFFECTS OF ZILPATEROL AND MELENGESTROL ACETATE ON BOVINE SKELETAL MUSCLE GROWTH AND DEVELOPMENT by ERIN KATHRYN SISSOM B.S., California State University, Fresno, 2002 M.S., Kansas State University, 2004 AN ABSTRACT OF A DISSERTATION submitted in partial fulfillment of the requirements for the degree DOCTOR OF PHILOSOPHY Department of Animal Sciences and Industry College of Agriculture KANSAS STATE UNIVERSITY Manhattan, Kansas 2009 Abstract Zilpaterol (ZIL) is a β-adrenergic receptor (β-AR) agonist that has been recently approved for use in feedlot cattle to improve production efficiencies and animal performance. One of the mechanisms through which this occurs is increased skeletal muscle growth. Therefore, two experiments were conducted to determine the effects of ZIL both in vivo and in vitro . In the first experiment, ZIL addition to bovine satellite cells resulted in a tendency to increase IGF-I mRNA and increased myosin heavy chain IIA (MHC) mRNA with 0.001 µ M and decreased MHC mRNA with 0.01 and 10 µ M. There were no effects of ZIL on protein synthesis or degradation. In myoblast cultures, there was a decrease in all three β-AR mRNA, and this was also reported in western blot analysis with a reduction in β2-AR expression due to ZIL treatment. In myotubes, there was an increase in β2-AR protein expression. In the second and third experiment, ZIL improved performance and carcass characteristics of feedlot steers and heifers. Additionally, ZIL decreased MHC IIA mRNA in semimembranosus muscle tissue collected from both steers and heifers. An additional part of the third study was conducted to determine the effects of melengestrol acetate (MGA) on bovine satellite cell and semimembranosus muscle gene expression.
    [Show full text]
  • Megestrol Acetate/Melengestrol Acetate 2115 Adverse Effects and Precautions Megestrol Acetate Is Also Used in the Treatment of Ano- 16
    Megestrol Acetate/Melengestrol Acetate 2115 Adverse Effects and Precautions Megestrol acetate is also used in the treatment of ano- 16. Mwamburi DM, et al. Comparing megestrol acetate therapy with oxandrolone therapy for HIV-related weight loss: similar As for progestogens in general (see Progesterone, rexia and cachexia (see below) in patients with cancer results in 2 months. Clin Infect Dis 2004; 38: 895–902. p.2125). The weight gain that may occur with meges- or AIDS. The usual dose is 400 to 800 mg daily, as tab- 17. Grunfeld C, et al. Oxandrolone in the treatment of HIV-associ- ated weight loss in men: a randomized, double-blind, placebo- trol acetate appears to be associated with an increased lets or oral suspension. A suspension of megestrol ace- controlled study. J Acquir Immune Defic Syndr 2006; 41: appetite and food intake rather than with fluid reten- tate that has an increased bioavailability is also availa- 304–14. tion. Megestrol acetate may have glucocorticoid ef- ble (Megace ES; Par Pharmaceutical, USA) and is Hot flushes. Megestrol has been used to treat hot flushes in fects when given long term. given in a dose of 625 mg in 5 mL daily for anorexia, women with breast cancer (to avoid the potentially tumour-stim- cachexia, or unexplained significant weight loss in pa- ulating effects of an oestrogen—see Malignant Neoplasms, un- Effects on carbohydrate metabolism. Megestrol therapy der Precautions of HRT, p.2075), as well as in men with hot 1-3 4 tients with AIDS. has been associated with hyperglycaemia or diabetes mellitus flushes after orchidectomy or anti-androgen therapy for prostate in AIDS patients being treated for cachexia.
    [Show full text]
  • Us Anti-Doping Agency
    2019U.S. ANTI-DOPING AGENCY WALLET CARDEXAMPLES OF PROHIBITED AND PERMITTED SUBSTANCES AND METHODS Effective Jan. 1 – Dec. 31, 2019 CATEGORIES OF SUBSTANCES PROHIBITED AT ALL TIMES (IN AND OUT-OF-COMPETITION) • Non-Approved Substances: investigational drugs and pharmaceuticals with no approval by a governmental regulatory health authority for human therapeutic use. • Anabolic Agents: androstenediol, androstenedione, bolasterone, boldenone, clenbuterol, danazol, desoxymethyltestosterone (madol), dehydrochlormethyltestosterone (DHCMT), Prasterone (dehydroepiandrosterone, DHEA , Intrarosa) and its prohormones, drostanolone, epitestosterone, methasterone, methyl-1-testosterone, methyltestosterone (Covaryx, EEMT, Est Estrogens-methyltest DS, Methitest), nandrolone, oxandrolone, prostanozol, Selective Androgen Receptor Modulators (enobosarm, (ostarine, MK-2866), andarine, LGD-4033, RAD-140). stanozolol, testosterone and its metabolites or isomers (Androgel), THG, tibolone, trenbolone, zeranol, zilpaterol, and similar substances. • Beta-2 Agonists: All selective and non-selective beta-2 agonists, including all optical isomers, are prohibited. Most inhaled beta-2 agonists are prohibited, including arformoterol (Brovana), fenoterol, higenamine (norcoclaurine, Tinospora crispa), indacaterol (Arcapta), levalbuterol (Xopenex), metaproternol (Alupent), orciprenaline, olodaterol (Striverdi), pirbuterol (Maxair), terbutaline (Brethaire), vilanterol (Breo). The only exceptions are albuterol, formoterol, and salmeterol by a metered-dose inhaler when used
    [Show full text]
  • Part I Biopharmaceuticals
    1 Part I Biopharmaceuticals Translational Medicine: Molecular Pharmacology and Drug Discovery First Edition. Edited by Robert A. Meyers. © 2018 Wiley-VCH Verlag GmbH & Co. KGaA. Published 2018 by Wiley-VCH Verlag GmbH & Co. KGaA. 3 1 Analogs and Antagonists of Male Sex Hormones Robert W. Brueggemeier The Ohio State University, Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, Columbus, Ohio 43210, USA 1Introduction6 2 Historical 6 3 Endogenous Male Sex Hormones 7 3.1 Occurrence and Physiological Roles 7 3.2 Biosynthesis 8 3.3 Absorption and Distribution 12 3.4 Metabolism 13 3.4.1 Reductive Metabolism 14 3.4.2 Oxidative Metabolism 17 3.5 Mechanism of Action 19 4 Synthetic Androgens 24 4.1 Current Drugs on the Market 24 4.2 Therapeutic Uses and Bioassays 25 4.3 Structure–Activity Relationships for Steroidal Androgens 26 4.3.1 Early Modifications 26 4.3.2 Methylated Derivatives 26 4.3.3 Ester Derivatives 27 4.3.4 Halo Derivatives 27 4.3.5 Other Androgen Derivatives 28 4.3.6 Summary of Structure–Activity Relationships of Steroidal Androgens 28 4.4 Nonsteroidal Androgens, Selective Androgen Receptor Modulators (SARMs) 30 4.5 Absorption, Distribution, and Metabolism 31 4.6 Toxicities 32 Translational Medicine: Molecular Pharmacology and Drug Discovery First Edition. Edited by Robert A. Meyers. © 2018 Wiley-VCH Verlag GmbH & Co. KGaA. Published 2018 by Wiley-VCH Verlag GmbH & Co. KGaA. 4 Analogs and Antagonists of Male Sex Hormones 5 Anabolic Agents 32 5.1 Current Drugs on the Market 32 5.2 Therapeutic Uses and Bioassays
    [Show full text]